hitch
#81
On Feb 12 (above) I commented about taking the poorly absorbed Siroboon with Grapefruit juice and how that might get the rapamycin blood level up to a reasonable level.
History:
I take 8mg Biocon Rapacan every week. Three times I’ve tested my rapamycin blood level after dosing, all of them two hours post consumption. Test 1 result was 17.1 ng/ml, Test 2 was 12.9 and test 3 was 31.9 (with GFJ).
Twice, I tried 8mg of the Siroboon 2mg pills (fewer pills seemed easier and cheaper).
First time I took it, my blood test came back at only 3.1 ng/ml (two hours post-dosing)
Second time my blood level was 3.8 after 2 hours and 3.2 after 6 hours.
As I still had a lot of Siroboon, I took 6mg with grapefruit juice on Monday (2 days ago). I had calculated that 6mg with GFJ would put my blood level around 12 ng/ml (based on my previous Biocon & GFJ test). My GFJ dosing was 3oz two hours before, 3oz twenty minutes before and 3oz when taking the Siroboon (this was the same as when I took GFJ with the Biocon and my blood level went up to 31.9).
My disappointing Siroboon results:
2 hours post dosing: 2.8 ng/ml
24 hours post dosing: <1 ng/ml (less than one)
Hard to believe the results were so bad. I don’t understand it. I do think that there actually is rapamycin in the Siroboon- as shown in a lab test posted on this site. So, I have to think that it has to do with absorption (maybe like the original 2009 mouse longevity study).
I’m throwing my seriously sucking Siroboon away!
5 Likes
hitch
#82
Additional thoughts about my poor Siroboon results from yesterday.
My conclusion is that the Siroboon 2mg Sirolimus must have an ineffective coating and is destroyed in the stomach, similar to the original 2009 mouse longevity study where they first used rapa with no coating. The consequence of this ineffective coating is that very little rapamycin enters the blood stream. This is demonstrated by my first two blood tests where the ng/ml was just 3.1 and 3.9.
This most recent blood test resulted in a blood level of 2.8 even though I took it with GFJ. GFJ does its work in the small intestine, blocking an enzyme that metabolizes (eats?) many drugs, including rapamycin. This blocking of metabolization means that more rapamycin is available to enter the bloodstream (like the 31.9 when I took the Biocon with GFJ). Apparently, almost no rapamycin entered my small intestine, so it must have been mostly destroyed by the stomach acid before it got there.
5 Likes
I took 6mg of Siroboon after 2 hours of 8oz GFJ and my 24 hour result was 3.2 ng/L. Next week I’ll try having the blood test 3 hours after the pill to get an idea of the peak.
What is the manufacturing date of your pack? Mine is September 2023.
2 Likes
hitch
#84
That’s very interesting and a big diff from my results. If you were at 3.2 after 24 hours, I’m guessing you must have had cMax of 8-14? I wonder if my GFJ was messed up- it had been in the freezer for four months?
Looks like I’ll have to try again with fresh GFJ…
1 Like
Yes - grapefruit juice could be a huge variance. Sometimes it works, sometimes it doesn’t, depending on the specific fruit and if juice, the juice processing approach.
For blood sirolimus tests, if you’re trying to see if the drug is actually working, I would not test with grapefruit juice because it could easily be the issue by itself.
Because different people produce varied amounts of the enzymes that break down sirolimus, the effect of grapefruit juice can vary, but tests of enzyme levels may be able to predict how an individual patient will respond.
“The variation in potency of the grapefruit juice itself may be far greater than the variation in the enzymes that break down sirolimus,” Cohen said. An early version of the study used canned grapefruit juice, generously donated by a Chicago-based grocery chain. But tests of the product found it lacked the active ingredients. So the researchers shifted to a frozen concentrate product supplied by the Florida Department of Citrus.
Source:
https://www.uchicagomedicine.org/forefront/news/grapefruit-juice-lets-patients-take-lower-dose-of-cancer-drug
1 Like
I’m going to have more blood test next week. 2-3 hours after and 7 days. And repeat in 2 weeks after. The GFJ I’ve are from the bottle in the supermarket. When I open the bottle, I freeze the rest of it in 250ml portions as they cannot keep long are opening.
What is the ideal or recommended peak level after 2 hours and 7 days? I’m definitely getting some side effects but not as bad as others described here.
hitch
#87
At 7 days (your trough) there should be <1 or 0 ng/ml
Nobody is certain what cMax should actually be!!! What I have seen most is between 12 and 18 ng/ml.
Others will have other opinions.
@RapAdmin - I don’t doubt GFJ can have great variations, but we are specifically testing Siroboon with GFJ…
2 Likes
Personally I feel that fresh grapefruit is the best way to get juice. Just eat a whole one.
4 Likes
Not available at the moment. I’ll try when they are at the shops.
@hitch what is your body weight? I’m about 110kg so maybe it make sense I need to increase my dosage.
hitch
#90
I’m 6’1" and 210 (95 kg). I’ve lost 15 pounds since I started taking rapa seven months ago. But I attribute most of the weight loss to exercise- when I started rapa, I also started doing two hours at the gym every other day.
Anyway, regarding dosage, RapAdmin did a poll on this site and the most common dosage was 6mg once per week. So, at 110kg, 8mg (10?) seems reasonable. But, we are all n=1 experimenters, taking a best (educated) guess on dosage.
4 Likes
I’ll get an idea of what the 2 hour and 7 days results are like before increasing my dosage. I’ll probably go 8mg and then 10mg. I don’t want it to spike beyond 30 ng/L.
1 Like
Alex
#92
What if we put the pills in a capsule? That should help right?
1 Like
SNK
#95
“seriously sucking” is the keyword here. My theory is simple. Never change something that works and RAPA from Biocon definitely works.
3 Likes
My second blood test. Had GFJ 2 hours before the 6mg dose. Now waiting for my turn for the blood test after 2 hours. Probably 2.5 hours when they draw my blood. Hope to get the results in 3 days.
I had the pills at 6.42am. and my blood was taken at 9.05am. so that means 2.3 hours later. Be interesting to see what I get this Friday.
2 Likes
I asked the local doctor to give me a script and they still refused. I’m stuck with this batch for now. What if I dip the pills in hemp oil before taking them? That should protect the pills longer? Lol
1 Like
SNK
#98
I doubt you’d get any benefit. Just take the damn pills alone or with GFJ. Simple.
SNK
#99
you don’t need a script. Your best script is talking to jagdish or anil and let them know how much you’d want to order. That’s all you need!
2 Likes
The border force in Australia restrict how much I can bring in. At the moment I’m not allowed to buy any until August. If the GP gives me a script, 100 x 1mg tablets will only cost me $29 at the local pharmacy. No GP in Australia will prescribe this medicine.
1 Like
